Synthesis And Antifungal Activity Of Novel Aryl ?-ketoesters

The pesticide is important to the developing of the world agricultural modernization. However, the extensive use of pesticide is harmful to the ecological environment. Meanwhile, with the increase of strengthening of people's environmental protection awareness and the worry of food safety, to develop the environmentally friendly, effective, low toxicity and residue compatible pesticides have become the subject of today's pesticide research. Pesticide intermediates are vital materials to product pesticides, they are paid more attention by chemical workers. To improve traditional synthetic methods of pesticide intermediates, make it more green and efficient, precisely conform to the theme of today's pesticide development.Aryl alpha-ketoesters are important medicine and pesticide intermediates, which have double functional groups. They can transform into many considerable compounds. The traditional methods to them often exist many disadvantages, such as harsh reaction conditions, complex reaction procedure and restrictive reaction rang. Accordingly, it is meaningful to research high efficient, simply and broad spectrum methods to synthetize them.This dissertation mainly developed a new method to synthesize ketoester compounds in one-pot with starting material of propiophenone acetophenone or benzoylformic acid, some of their biological activities were also screened, expecting to find new biological activity compounds.The main achievements are described in the following five aspects:1. To explore the method of using propiophenone, acetophenone or benzoylformic acid as raw materials in the role of oxygen, synthesis aryl ?-ketoesters in one-pot. The resulting compounds have all been verified by high resolution mass spectrometry, 1~H and (13)~ C NMR;2. The reaction conditions have been optimized and the yields were improved under the optimal reaction condition;3. The scope of the substrates was extended to explore the broad spectrum of the reactions;4. To explore the course of this type reaction was studied and put forward possible mechanism of this type of reaction, and then test and verify the assume;5. To determinate of antifungal activity of some new compounds. In conclusion, a novel, simple and efficient method of synthesizing aryl ?-ketoesters has been developed, and 23 new aryl ?-ketoesters which have not been reported in the literature before we synthesized. The course used inexpensive, abundant and environmentally friendly molecular oxygen as oxidant, at the same time, the reaction possesses good regioselectivity. To determinate of antifungal activity of some new compounds, and obtain certain results.